Lodoxamide - Histamine Receptor 抑制剂 - 生命科学试剂 - MedChemExpress_第1页
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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELodoxamideCat. No.: HY-14270CAS No.: 53882-12-5分式: CHClNO分量: 311.63作靶点: Histamine Receptor作通路: GPCR/G Protein; Immunology/Inflammation; NeuronalSignaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据

2、体外实验 DMSO : 30 mg/mL (96.27 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.2089 mL 16.0447 mL 32.0893 mL5 mM 0.6418 mL 3.2089 mL 6.4179 mL10 mM 0.3209 mL 1.6045 mL 3.2089 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Lodoxamide作

3、为肥细胞稳定剂的抗过敏化合物, 于治疗哮喘和过敏性结膜炎的。体外研究Lodoxamide inhibits compound 48/80-induced histamine release and ionophore-induced 45Ca influx withassociated histamine release in purified rat peritoneal mast cells 1. The chemotactic response ofeosinophils to fMLP as well as to IL-5 is significant and dose-depende

4、nt inhibited by Lodoxamide.1/2 Master of Small Molecules 您边的抑制剂师www.MedChemELodoxamide is also able to strongly inhibit the release of eosinophil peroxidase after IgA-dependentactivation and, to a lesser extent, the release of eosinophil cationic protein and eosinophil-derived neurotoxin2.体内研究 Lodox

5、amide has been demonstrated to have cromolyn-like activity when studied in the rat peritoneal mastcell assay (PCA) model3 and in Ascaris antigen-sensitized rhesus monkeys. When given intravenously,orally, or intrabronchially by aerosol, lodoxamide significantly inhibits the increased respiratory fre

6、quency anddecreased tidal volume induced by antigen challenge in Ascaris-sensitized. anesthetized rhesus monkeys1. Addition of lodoxamide tromethamine to Euro-Collins or University of Wisconsin solution results in amarked decrease in lung reperfusion injury as demonstrated by increased oxygenation,

7、decreasedmicrovascular permeability, and increased compliance 3. Patients treated with lodoxamide tromethaminedemonstrate an improvement in daytime breathing difficulty, cough, sputum production, and sleep 4.REFERENCES1. Watt GD, et al. Protective effect opf lodoxamide tromethamine on allergen inhal

8、ation challenge. J Allergy Clin Immunol. 1980Oct;66(4):286-94.2. Capron M,et al. Inhibitory effects of lodoxamide on eosinophil activation. Int Arch Allergy Immunol. 1998 Jun;116(2):140-6.3. Barr ML, et al. Addition of a mast cell stabilizing compound to organ preservation solutions decreases lung r

9、eperfusion injury. J ThoracCardiovasc Surg. 1998 Mar;115(3):631-6; discussion 636-7.4. Mann JS, et al. Inhaled lodoxamide tromethamine in the treatment of perennial asthma: a double-blind placebo-controlled study. JAllergy Clin Immunol. 1985 Jul;76(1):83-90.McePdfHeightCaution: Product has not been fully validated for medical

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